发明名称 ANILIDE DERIVATIVES
摘要 Compounds are described of general formula (I) and salts and solvates thereof, including physiologically acceptable salts and solvates thereof, in which: Z represents either Het, (a), or (b); Het represents an optionally substituted bicyclic or tricyclic ring selected from quinolin-4-yl, isoquinolin-1-yl, isoquinolin-3-yl, quinolin-3-yl, quinolin-2-yl, quinoxalin-2-yl, naphthalen-1-yl, naphthalen-2-yl, indol-2-yl, 4-oxo-4H-1-benzopyran-2-yl, phenazin-1-yl and phenothiazin-1-yl or an aryl substituted monocyclic ring selected from 2-aryl-4-thiazolyl, 2-aryl-5-thiazolyl, 5-aryl-2-thienyl, 2-aryl-4-triazolyl and 1-aryl-4-pyrazolyl where aryl represents a phenyl or pyridyl ring optionally substituted by a halogen atom or a trifluoromethyl, C1-4 alkyl or C1-4 alkoxy group. The above-mentioned bicyclic or tricyclic rings may be unsubstituted or substituted by one, two or three groups selected from C1-4 alkyl and C1-4 alkoxy. Quinolin-4-yl rings may also be substituted in the ring 2 position by phenyl or phenyl substituted by C1-4 alkoxy. Indol-2-yl rings may also be substituted in the ring 3 position by benzoyl; R8 represents a hydrogen or halogen atom or a C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, amino or nitro group; p represent 1; or when R8 represents C1-4 alkoxy p may also represent 2 or 3; R9 represents a hydrogen or halogen atom or a C1-4 alkyl, C1-4 alkoxy or C1-4 alkylthio group; R10 and R11 may each represent a hydrogen atom or together form a bond or a linking atom selected from -O- or -S-; and X represents an oxygen atom or NR12 (where R12 represents a hydrogen atom or a C1-4 alkyl group). The novel compounds of formula (I) can sensitize multi-drug resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an anti-tumour drug.
申请公布号 WO9401408(A1) 申请公布日期 1994.01.20
申请号 WO1993EP01802 申请日期 1993.07.08
申请人 LABORATOIRES GLAXO S.A. 发明人 DUMAITRE, BERNARD, ANDRE;DODIC, NERINA;DAUGAN, ALAIN, CLAUDE-MARIE;PIANETTI, PASCAL, MAURICE, CHARLES
分类号 A61K31/165;A61K31/35;A61K31/352;A61K31/38;A61K31/382;A61K31/425;A61K31/426;A61K31/47;A61K31/472;A61K31/54;A61K31/5415;A61P35/00;C07C233/70;C07C233/75;C07C233/80;C07C235/84;C07D209/42;C07D215/48;C07D215/52;C07D215/54;C07D217/02;C07D217/04;C07D217/18;C07D217/26;C07D241/44;C07D241/46;C07D277/20;C07D277/56;C07D279/20;C07D311/86;C07D335/16;C07D401/12;C07D405/12;C07D409/12;C07D409/14;C07D417/12;C07D417/14;(IPC1-7):C07D217/04 主分类号 A61K31/165
代理机构 代理人
主权项
地址